Assay Detail
Binding
CHEMBL760946
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of phosphodiesterase 1/5 isozyme (PDE1/5) mixture isolated from the guinea pig trachea.
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Trachea |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 4.44 | 5.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL145499 | — | — | 1 | 5.46 |
| CHEMBL144258 | — | — | 1 | 5.28 |
| CHEMBL436207 | — | — | 1 | 4.85 |
| CHEMBL434838 | — | — | 1 | 4.79 |
| CHEMBL418848 | — | — | 1 | 4.79 |
| CHEMBL357197 | — | — | 1 | 4.52 |
| CHEMBL341662 | — | — | 1 | 4.47 |
| CHEMBL341671 | — | — | 1 | 4.42 |
| CHEMBL145390 | — | — | 1 | 4.41 |
| CHEMBL339749 | — | — | 1 | 4.30 |
| CHEMBL357616 | — | — | 1 | 4.27 |
| CHEMBL126581 | — | — | 1 | 4.18 |
| CHEMBL423931 | — | — | 1 | 4.17 |
| CHEMBL144245 | — | — | 1 | 4.14 |
| CHEMBL111925 | — | — | 1 | 4.13 |
| CHEMBL144404 | — | — | 1 | 4.04 |
| CHEMBL434516 | — | — | 1 | 4.03 |
| CHEMBL144570 | — | — | 1 | 4.03 |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 4.02 |
| CHEMBL125828 | — | — | 1 | - |
| CHEMBL422653 | — | — | 1 | - |
| CHEMBL339408 | — | — | 1 | - |
| CHEMBL422828 | — | — | 1 | - |
| CHEMBL112366 | — | — | 1 | - |
| CHEMBL146218 | — | — | 1 | - |
| CHEMBL343243 | — | — | 1 | - |
| CHEMBL144452 | — | — | 1 | - |
| CHEMBL145258 | — | — | 1 | - |
| CHEMBL125671 | — | — | 1 | - |
| CHEMBL125123 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL145499 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL144258 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL436207 | — | IC50 | = | 14100.0 | nM | 4.85 |
| CHEMBL434838 | — | IC50 | = | 16100.0 | nM | 4.79 |
| CHEMBL418848 | — | IC50 | = | 16100.0 | nM | 4.79 |
| CHEMBL357197 | — | IC50 | = | 30100.0 | nM | 4.52 |
| CHEMBL341662 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL341671 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL145390 | — | IC50 | = | 39200.0 | nM | 4.41 |
| CHEMBL339749 | — | IC50 | = | 50600.0 | nM | 4.30 |
| CHEMBL357616 | — | IC50 | = | 53300.0 | nM | 4.27 |
| CHEMBL126581 | — | IC50 | = | 65300.0 | nM | 4.18 |
| CHEMBL423931 | — | IC50 | = | 67700.0 | nM | 4.17 |
| CHEMBL144245 | — | IC50 | = | 72000.0 | nM | 4.14 |
| CHEMBL111925 | — | IC50 | = | 73400.0 | nM | 4.13 |
| CHEMBL144404 | — | IC50 | = | 90700.0 | nM | 4.04 |
| CHEMBL144570 | — | IC50 | = | 93200.0 | nM | 4.03 |
| CHEMBL434516 | — | IC50 | = | 93200.0 | nM | 4.03 |
| CHEMBL63 | ROLIPRAM | IC50 | = | 94900.0 | nM | 4.02 |
| CHEMBL144370 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL342285 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL144605 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL356548 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL144287 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL125123 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL125671 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL145258 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL144452 | — | IC50 | = | - | nM | - |
| CHEMBL343243 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL146218 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL112366 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL422828 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL339408 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL422653 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL125828 | — | IC50 | > | 100000.0 | nM | - |